Abstract: The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or “chiral tetralone.” The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).

Abstract: This invention relates to methods of preparing compounds of Formula 1: and to pharmaceutically acceptable salts and solvates thereof, and to methods for preparing same. The compounds of Formula 1 are antibacterial agents that may be used to treat various bacterial and protozoal infections, and may also be used to treat cancer. The invention also relates to pharmaceutical compositions comprising the compounds of Formula 1, and to methods of treating sbacterial and protozoal infections by administering compounds of Formula 1.